Rapamycin-13C,d3
Rapamycin-13C,d3 (Sirolimus-13C,d3) is the 13C, deuterated-labeled Rapamycin (HY-10219). Rapamycin (Sirolimus; AY 22989) is a potent and specific blood-brain barrier-transmissible mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells. Rapamycin is a molecular glue that binds FKBP12 and mTOR proteins together, thereby inhibiting mTOR kinase activity. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1. Rapamycin is an autophagy activator, an immunosuppressant.
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- Pureté: 97.05%
- Formule: C5013CH76D3NO13
- Masse moléculaire:918.18
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Stockage:
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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mTOR 0.1 nM (IC50, in HEK293 cells ) |
Microbial Metabolite |
FKBP12 |
Autophagy |
Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Lung cancer cell lines A549, SPC-A-1, 95D and NCI-H446
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Concentration:12.5 nM, 25 nM, 50 nM, 100 nM
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Incubation Time:24 hours
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Result:Treatment exerted modest inhibitory effect on lung cancer cell proliferation in a dose-dependent manner in all cell lines.
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Cell Line:95D cells
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Concentration:10 nM and 20 nM
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Incubation Time:24 hours
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Result:Combination treatment with RP-56976 decreased phosphorylation of ERK.
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Animal Model:24 male nu/nu mice aged 4-5 week old (15-20 g)[4]
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Dosage:2.0 mg/kg
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Administration:Intraperitoneal injection; every other day; 28 days
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Result:Had a moderate inhibitory effect in monotherapy group. The combination with Metformin exerted a significantly increased inhibition of tumor growth.
1. This compound can be used as a tracer
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.
Chemical Information
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Unlabeled Cas 53123-88-9
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Appearance Solid
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Masse moléculaire 918.18
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Formule C5013CH76D3NO13
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Color White to off-white
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SMILES
O=C([C@@]1(O)[C@@H](CC[C@@H](C[C@@H](/C(C)=C/C=C/C=C/[C@H](C[C@@H](C)C([C@@H]([C@@H](/C(C)=C/[C@H]2C)O)OC)=O)C)O[13C]([2H])([2H])[2H])O1)C)C(N3CCCC[C@H]3C(O[C@@H](CC2=O)[C@@H](C[C@H]4C[C@H]([C@H](O)CC4)OC)C)=O)=O
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Synonyms
Sirolimus-13C,d3; AY-22989-13C,d3 NSC 226080-13C,d3
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Pureté et documentation
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Fiche technique (281 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Edwards SR, et al. The rapamycin-binding domain of the protein kinase mammalian target of rapamycin is a destabilizing domain. J Biol Chem, 2007, 282(18), 13395-13401. [Content Brief]
[2]. Rangaraju S, et al. Rapamycin activates autophagy and improves myelination in explant cultures from neuropathicmice. J Neurosci. 2010 Aug 25;30(34):11388-97. [Content Brief]
[3]. Niu H, et al. Rapamycin potentiates cytotoxicity by RP-56976 possibly through downregulation of Survivin in lung cancer cells. J Exp Clin Cancer Res. 2011 Mar 10;30:28. [Content Brief]
[4]. Zhang JW, et al. Metformin synergizes with rapamycin to inhibit the growth of pancreatic cancer in vitro and in vivo. Oncol Lett. 2018 Feb;15(2):1811-1816. [Content Brief]
[5]. Svensson JE, et al. Evaluating the effect of rapamycin treatment in Alzheimer's disease and aging using in vivo imaging: the ERAP phase IIa clinical study protocol. BMC Neurol. 2024 Apr 4;24(1):111. [Content Brief]
[6]. Soini L, et al. Molecular glues to stabilise protein-protein interactions. Curr Opin Chem Biol. 2022 Aug;69:102169. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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